Antitrypanosomal, antileishmanial, and antimalarial activities of quaternary arylalkylammonium 2-amino-4-chlorophenyl phenyl sulfides, a new class of trypanothione reductase Inhibitor, and of n-acyl derivatives of 2-amino-4 chlorophenyl phenyl sulfide

by Parveen S, Khan MO, Austin SE, Croft SL, Yardley V, Rock P, Douglas KT. J Med Chem, December 2005, 48(25):8087-97.

Summary: Quaternization of the nitrogen atom of 2-amino-4-chlorophenyl phenyl sulfide analogues of chlorpromazine improved inhibition ~40-fold (3’,4’-dichlorobenzyl-[5-chloro-2 phenylsulfanylphenylamino)-propyl]-dimethylammonium chloride inhibited trypanothione reductase from Trypanosoma cruzi with a linear competitive Ki value of 1.7 ( 0.2 íM). The phenothiazine and diaryl sulfide quaternary compounds were also powerful antimalarials, providing a new structural framework for antimalarial design.

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